Research Article | Volume: 7, Issue: 8, August, 2017

Design, Synthesis and biological evaluation of some novel indole derivatives as selective COX-2 inhibitors

Khaled R. A. Abdellatif Mohammed T. Elsaady Noha.H.Amin Ahmed A. Hefny   

Open Access   

Published:  Aug 30, 2017

DOI: 10.7324/JAPS.2017.70810

A new group of (4-substitutedphenyl)(3-((2-(4- substitutedphenyl)hydrazono)methyl)-1H-indol-1-yl)methanone derivatives 13a-f as indomethacin analogs was synthesized through N-benzoylation of indole-3-cabaldehyde with the appropriate benzoyl fragment followed by reaction with substituted phenylhydrazine. All the synthesized compounds were evaluated in vitro for COX-1/COX-2 inhibitory activity and in vivo for their anti-inflammatory activity in comparison with the parent drug indomethacin. Compounds 13a,b,d,e which contain SO2Me or SO2NH2 group as a pharmacophore of COX-2, exhibited the most anti-inflammatory and selectivity actives so, they were more evaluated by calculating their ED50% doses and ulcerogenic indices to ensure their gastric safety margin relative to indomethacin.

Keyword:     NSAIDS Cyclooxygenase IndomethacinAnti-inflammatory activity Ulcerogenicity.


Abdellatif KRA, Elsaady MT, Amin NH, Hefny AA. Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and gastric liability of some novel indole derivatives as a selective COX-2 inhibitors. J App Pharm Sci, 2017; 7 (08): 069-077.

Copyright: © The Author(s). This is an open-access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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